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[含盐酸罂粟碱栓剂的处方设计与分析。第1部分。最佳基质的选择及栓剂物理参数的测定]

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 1. Choice of the optimal vehicle and determination of the physical parameters of the suppositories].

作者信息

Regdon G, Vastag T, Regdon G, Selmeczi B

机构信息

Szent-Györgyi Albert Orvostudományi Egyetem, Gyógyszertechnológiai Intézet, Szeged.

出版信息

Acta Pharm Hung. 1991 Nov;61(6):295-302.

PMID:1785358
Abstract

Suppositories containing 0.10 g papaverine hydrochloride were made with moulding technology to produce spasmolytic effect. The optimal vehicle was tried to be found for these suppositories. During the experiments 12 different suppository masses were used, including lipophil and lipohydrophil vehicles as well as vehicles with low and high hydroxyl numbers. Five different kinds of physical parameters were determined: melting and drop points, disintegration and special penetration times and breaking hardness. The physical parameters of suppositories without active substance and containing papaverine were examined separately. After 6 months of storage the greater part of the masses showed unfavourable changes (after-hardening, increase of the disintegration time, etc.). In the end the Estaram 299 mass, a triglyceride type of mass with a low hydroxyl number was found satisfactory in every respect, either in itself or combined with 5% Estasan neutral oil.

摘要

采用成型技术制备含0.10 g盐酸罂粟碱的栓剂以产生解痉作用。试图为这些栓剂找到最佳基质。实验过程中使用了12种不同的栓剂基质,包括亲脂性和亲水性基质以及羟值低和高的基质。测定了五种不同的物理参数:熔点和滴点、崩解时间和特定穿透时间以及破裂硬度。分别检查了不含活性物质和含罂粟碱的栓剂的物理参数。储存6个月后,大部分基质出现了不利变化(硬化后、崩解时间增加等)。最后发现,羟值低的甘油三酯型基质Estaram 299,无论单独使用还是与5%的Estan中性油混合,在各方面都令人满意。

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